An Improved and Scalable Process for the Synthesis of Ezetimibe: An Antihypercholesterolemia Drug

An efficient, cost-effective and large-scale synthesis of ezetimibe 1, an antihypercholesterolemia drug, is described. Chiral oxazolidinone chemistry was used to fix the required stereochemistry of the β-lactam ring, and the chiral oxazaborolidine chemistry was used to fix the hydroxyl group stereoc...

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Bibliographic Details
Published in:Organic process research & development 2009-09, Vol.13 (5), p.907-910
Main Authors: Sasikala, C. H. V. A, Reddy Padi, Pratap, Sunkara, Vishnuvardhan, Ramayya, Pattabhi, Dubey, P. K, Bhaskar Rao Uppala, Venkata, Praveen, Cherukupally
Format: Article
Language:English
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Summary:An efficient, cost-effective and large-scale synthesis of ezetimibe 1, an antihypercholesterolemia drug, is described. Chiral oxazolidinone chemistry was used to fix the required stereochemistry of the β-lactam ring, and the chiral oxazaborolidine chemistry was used to fix the hydroxyl group stereochemistry. The synthesis significantly lowers the cost and provides easy access to ezetimibe on large scale.
ISSN:1083-6160
1520-586X
DOI:10.1021/op900039z